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Assay Detail

CHEMBL4618315

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of NanoBRET kinase tracer K4 binding to full-length human C-terminal NanoLuc-tagged p38alpha MAPK expressed in HEK293T cells incubated for 2 hrs by NanoBRET NanoGlo substrate based NanoBRET assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mitogen-activated protein kinase 14 (CHEMBL260)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Bioisosteric Replacement of Arylamide-Linked Spine Residues with N-Acylhydrazones and Selenophenes as a Design Strategy to Novel Dibenzosuberone Derivatives as Type I 1/2 p38α MAP Kinase Inhibitors.
Pedreira JGB, Nahidino P, Kudolo M, Pantsar T, Berger BT, Forster M, Knapp S, Laufer S, Barreiro EJ.
J Med Chem (2020) 63 : 7347 -7354
PubMed 32462866 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.04 8.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2316207 FS-694 1 8.37
CHEMBL4646557 1 8.31
CHEMBL4640746 1 8.20
CHEMBL4645084 1 7.81
CHEMBL4642910 1 7.52
CHEMBL4648755 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2316207 FS-694 IC50 = 4.3 nM 8.37
CHEMBL4646557 IC50 = 4.9 nM 8.31
CHEMBL4640746 IC50 = 6.3 nM 8.20
CHEMBL4645084 IC50 = 15.5 nM 7.81
CHEMBL4642910 IC50 = 30.4 nM 7.52
CHEMBL4648755 IC50 - -